Found 3 hits Enz. Inhib. hit(s) with Target = 'Glucagon receptor' and Ligand = 'BDBM50007451' Target/Host
(Institution) | Ligand | Target/Host
Links | Ligand
Links | Trg + Lig
Links | Ki
nM | ΔG°
kJ/mole | IC50
nM | Kd
nM | EC50/IC50
nM | koff
s-1 | kon
M-1s-1 | pH | Temp
°C |
|---|
Glucagon receptor
(Homo sapiens (Human)) | BDBM50007451
(CHEMBL3237921)Show SMILES CC(C)(C)[C@H]1CC[C@]2(CC1)N=C(C(=O)N2[C@H](C1CC1)c1ccc(cc1)C(=O)NCc1nn[nH]n1)c1cc(Cl)cc(Cl)c1 |r,wU:4.3,15.17,wD:7.6,c:11,(3.48,-8.51,;4.67,-9.5,;3.22,-10.03,;4.41,-11.01,;6.11,-8.96,;6.37,-7.45,;7.82,-6.91,;9,-7.9,;8.74,-9.42,;7.29,-9.95,;9.42,-6.42,;10.96,-6.36,;11.49,-7.81,;12.97,-8.22,;10.28,-8.76,;10.34,-10.3,;9.01,-11.08,;7.47,-11.11,;8.26,-12.43,;11.66,-11.08,;11.64,-12.63,;12.97,-13.41,;14.31,-12.66,;14.33,-11.12,;13.01,-10.33,;15.64,-13.45,;15.61,-14.99,;16.97,-12.7,;18.3,-13.48,;19.64,-12.73,;21.04,-13.36,;22.08,-12.23,;21.33,-10.89,;19.82,-11.19,;11.74,-5.03,;10.98,-3.7,;11.75,-2.37,;10.99,-1.03,;13.29,-2.37,;14.06,-3.71,;15.6,-3.72,;13.28,-5.04,)| Show InChI InChI=1S/C31H35Cl2N7O2/c1-30(2,3)22-10-12-31(13-11-22)35-26(21-14-23(32)16-24(33)15-21)29(42)40(31)27(18-4-5-18)19-6-8-20(9-7-19)28(41)34-17-25-36-38-39-37-25/h6-9,14-16,18,22,27H,4-5,10-13,17H2,1-3H3,(H,34,41)(H,36,37,38,39)/t22-,27-,31-/m1/s1 | PDB
MMDB
UniProtKB/SwissProt
B.MOAD
antibodypedia
GoogleScholar
AffyNet 
| CHEMBL
PC cid
PC sid
UniChem
Patents
Similars
| Article
PubMed
| n/a | n/a | 72 | n/a | n/a | n/a | n/a | n/a | n/a |
Merck Research Laboratories
Curated by ChEMBL
| Assay Description
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis |
J Med Chem 57: 2601-10 (2014)
Article DOI: 10.1021/jm401858f
BindingDB Entry DOI: 10.7270/Q20V8F9P |
More data for this
Ligand-Target Pair | |
Glucagon receptor
(Homo sapiens (Human)) | BDBM50007451
(CHEMBL3237921)Show SMILES CC(C)(C)[C@H]1CC[C@]2(CC1)N=C(C(=O)N2[C@H](C1CC1)c1ccc(cc1)C(=O)NCc1nn[nH]n1)c1cc(Cl)cc(Cl)c1 |r,wU:4.3,15.17,wD:7.6,c:11,(3.48,-8.51,;4.67,-9.5,;3.22,-10.03,;4.41,-11.01,;6.11,-8.96,;6.37,-7.45,;7.82,-6.91,;9,-7.9,;8.74,-9.42,;7.29,-9.95,;9.42,-6.42,;10.96,-6.36,;11.49,-7.81,;12.97,-8.22,;10.28,-8.76,;10.34,-10.3,;9.01,-11.08,;7.47,-11.11,;8.26,-12.43,;11.66,-11.08,;11.64,-12.63,;12.97,-13.41,;14.31,-12.66,;14.33,-11.12,;13.01,-10.33,;15.64,-13.45,;15.61,-14.99,;16.97,-12.7,;18.3,-13.48,;19.64,-12.73,;21.04,-13.36,;22.08,-12.23,;21.33,-10.89,;19.82,-11.19,;11.74,-5.03,;10.98,-3.7,;11.75,-2.37,;10.99,-1.03,;13.29,-2.37,;14.06,-3.71,;15.6,-3.72,;13.28,-5.04,)| Show InChI InChI=1S/C31H35Cl2N7O2/c1-30(2,3)22-10-12-31(13-11-22)35-26(21-14-23(32)16-24(33)15-21)29(42)40(31)27(18-4-5-18)19-6-8-20(9-7-19)28(41)34-17-25-36-38-39-37-25/h6-9,14-16,18,22,27H,4-5,10-13,17H2,1-3H3,(H,34,41)(H,36,37,38,39)/t22-,27-,31-/m1/s1 | PDB
MMDB
UniProtKB/SwissProt
B.MOAD
antibodypedia
GoogleScholar
AffyNet
| CHEMBL
PC cid
PC sid
UniChem
Patents
Similars
| Article
PubMed
| n/a | n/a | 540 | n/a | n/a | n/a | n/a | n/a | n/a |
Merck Research Laboratories
Curated by ChEMBL
| Assay Description
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins follo... |
J Med Chem 57: 2601-10 (2014)
Article DOI: 10.1021/jm401858f
BindingDB Entry DOI: 10.7270/Q20V8F9P |
More data for this
Ligand-Target Pair | |
Glucagon receptor
(Mus musculus) | BDBM50007451
(CHEMBL3237921)Show SMILES CC(C)(C)[C@H]1CC[C@]2(CC1)N=C(C(=O)N2[C@H](C1CC1)c1ccc(cc1)C(=O)NCc1nn[nH]n1)c1cc(Cl)cc(Cl)c1 |r,wU:4.3,15.17,wD:7.6,c:11,(3.48,-8.51,;4.67,-9.5,;3.22,-10.03,;4.41,-11.01,;6.11,-8.96,;6.37,-7.45,;7.82,-6.91,;9,-7.9,;8.74,-9.42,;7.29,-9.95,;9.42,-6.42,;10.96,-6.36,;11.49,-7.81,;12.97,-8.22,;10.28,-8.76,;10.34,-10.3,;9.01,-11.08,;7.47,-11.11,;8.26,-12.43,;11.66,-11.08,;11.64,-12.63,;12.97,-13.41,;14.31,-12.66,;14.33,-11.12,;13.01,-10.33,;15.64,-13.45,;15.61,-14.99,;16.97,-12.7,;18.3,-13.48,;19.64,-12.73,;21.04,-13.36,;22.08,-12.23,;21.33,-10.89,;19.82,-11.19,;11.74,-5.03,;10.98,-3.7,;11.75,-2.37,;10.99,-1.03,;13.29,-2.37,;14.06,-3.71,;15.6,-3.72,;13.28,-5.04,)| Show InChI InChI=1S/C31H35Cl2N7O2/c1-30(2,3)22-10-12-31(13-11-22)35-26(21-14-23(32)16-24(33)15-21)29(42)40(31)27(18-4-5-18)19-6-8-20(9-7-19)28(41)34-17-25-36-38-39-37-25/h6-9,14-16,18,22,27H,4-5,10-13,17H2,1-3H3,(H,34,41)(H,36,37,38,39)/t22-,27-,31-/m1/s1 | PDB
KEGG
UniProtKB/SwissProt
B.MOAD
GoogleScholar
AffyNet
| CHEMBL
PC cid
PC sid
UniChem
Patents
Similars
| Article
PubMed
| n/a | n/a | 750 | n/a | n/a | n/a | n/a | n/a | n/a |
Merck Research Laboratories
Curated by ChEMBL
| Assay Description
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis |
J Med Chem 57: 2601-10 (2014)
Article DOI: 10.1021/jm401858f
BindingDB Entry DOI: 10.7270/Q20V8F9P |
More data for this
Ligand-Target Pair | |
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